Abstract: Pyranoside derivatives of the formula I
wherein 1, m and n independently of one another denote an integer chosen from 0, 1, 2, 3 and 4 and 1+m+n≦4. These are are LTB4-antagonists. Also disclosed are processes for making these compounds.
Type:
Grant
Filed:
March 8, 1999
Date of Patent:
March 6, 2001
Assignee:
Boehringer Ingelheim KG
Inventors:
Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans M. Jennewein, Christopher J. M. Meade, Andreas Ding
Abstract: A composition and method of treating skin ulcers utilizes a combination of sucralfate and a topical anesthetic such as lidocaine. The composition finds utility in treating the symptoms of d from herpes, acne, psoriasis, eczema, diabetic ulcers, bed sores, shingles, jock itch, athlete's foot, ringworm, and other dermal conditions. The composition also finds utility in preventing the development of nascent herpes outbreaks into herpes ulcers, in addition to providing long-lasting relief from such symptoms.
Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.
Abstract: A compound effect for the treatment of dermatological disorders comprises a mono- or diester of an &agr;,&ohgr;-dicarboxylic acid, wherein the alcohol moiety of the said ester comprises a keratolytically active alcohol. The compound may have the formula,
where n is in the range of 6 to 12; m is in the range of 0 to 8; R′ is selected from the group consisting of H, alkyl, aryl, alkenyl, benzyl, OH, NHR″, CONHR″ and COOR″; R″ is selected from the group consisting of alkyl, aryl, alkenyl, and benzyl; and Y is selected from the group consisting of H, alkyl, aryl, alkenyl, benzyl and X.
Abstract: The present invention relates to self-tanning compositions comprising an effective amount of DHA in combination with an effective amount of propolis extract. The compositions provide self-tanning compositions which can produce a tan with enhanced coloration. The self-tan produced using the compositions of the present invention is more natural looking. In another embodiment of the present invention, the compositions comprise DHA combined with caffeic acid phenethyl ester.
Type:
Grant
Filed:
July 8, 1999
Date of Patent:
January 9, 2001
Assignee:
Color Access, Inc.
Inventors:
Andrew J. Bevacqua, Konstantinos M. Lahanas, Neelam Muizzuddin, Nicolae Vrabie
Abstract: A pesticidal device which comprises a pesticidal ingredient being volatile at room temperature (e.g. 1-ethynyl-2-methyl-2-pentenyl 3-(2-chloro-2-fluorovinyl)-2,2-dimethylcyclopropanecarboxylate, 1-ethynyl-2-fluoro-2-pentenyl 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate), 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(2-methyl-1-propenyl)-2,2-dimethylcyclopropanecarboxylate, 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(2-chloro-2-fluorovinyl)-2,2-dimethylcyclopropanecarboxylate, 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(1-propenyl)-2,2-dimethylcyclopropanecarboxylate) is supported on balloon material, and a method for controlling pests by using the pesticidal device.
Abstract: A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.
Type:
Grant
Filed:
September 4, 1998
Date of Patent:
December 19, 2000
Assignee:
The Regents of the University of California
Inventors:
Dennis A. Carson, Hsien C. Shih, Howard B. Cottam, Lorenzo Leoni
Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.
Abstract: The present invention is directed to fungicidal compositions for agricultural and horticultural use, characterized in that the composition comprises a benzamidoxime composed represented by a general formula [I]: ##STR1## wherein R.sup.1 represents alkyl, alkenyl, etc., R.sup.2 represents phenyl, heterocycle, etc., X.sup.1 represents haloalkyl, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 each independently represent hydrogen, halogeno, alkyl, etc., r.sub.1 and r.sub.2 each independently represent hydrogen, halogeno, alkyl, etc., and a so-called acrylate fungicide as the active ingredients. The fungicidal compositions according to the present invention are combination compositions of fungicidal components, which can improve fungicidal activity obtainable with each component in the combination with a less dose in total of each components.
Abstract: Compounds that are isolatable from cherries and have antioxidant activity, and methods for isolating these compounds are described. In particular, the invention relates to 1-(3',4'-dihydroxycinnamoyl)-cyclopenta-2,3-diol and 1-(3',4'-dihydroxycinnamoyl)-cyclopenta-2,5-diol, which have antioxidant activity. These antioxidant compounds and compositions containing these compounds are useful as food preservatives, dietary supplements, nutraceuticals, and phytoceuticals.
Type:
Grant
Filed:
June 10, 1999
Date of Patent:
November 21, 2000
Assignee:
Board of Trustees operating Michigan State University
Inventors:
Muraleedharan G. Nair, Haibo Wang, Gale M. Strasburg, Alden M. Booren, James I. Gray
Abstract: The present invention relates to methods for effectively inhibiting unwanted angiogenesis. More particularly, this invention relates to methods of treating diseases that show unwanted angiogenesis and to delivering anti-angiogenic activity to a mammal. In other aspects this invention relates to methods of reducing the level of tumor necrosis factor .alpha..
Type:
Grant
Filed:
March 22, 1999
Date of Patent:
November 21, 2000
Assignees:
Large Scale Biology Corporation, SRI International
Inventors:
Daniel Tuse, Charles Hiebert, Keith R. Laderoute, Nahid Waleh
Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.
Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.
Abstract: Cyclopentenone derivative having a structure of 5-(R.sub.1 COO--)-4-(R.sub.2 COO--)--substituted 2-cyclopenten-1-one (R.sub.1 and R.sub.2 are some or different and each is alkyl group, alkenyl group or aryl group) or an optically active substance thereof; a method for the manufacture of the cyclopentenone derivative by the reaction of 4,5-dihydroxy-2-cyclopenten-1-one with the corresponding carboxylic acid or a reactive derivative thereof; and anticancer agent, apoptosis-inducing agent and antibacterial agent containing said derivative.
Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
September 12, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Cornelia J. Forster
Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.
Type:
Grant
Filed:
March 11, 1997
Date of Patent:
August 29, 2000
Assignee:
Beacon Laboratories, Inc.
Inventors:
Abraham Nudelman, Ada Rephaeli, Edward Neiss, Bernard Loev
Abstract: The present invention relates to dimethyl-substituted cyclohexanediene derivatives, to a process for their preparation, to their use as pharmaceuticals and to corresponding pharmaceuticals.
Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Type:
Grant
Filed:
February 7, 1997
Date of Patent:
July 18, 2000
Assignee:
Emisphere Technologies, Inc.
Inventors:
Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Harry R. Leipold
Abstract: Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.
Abstract: Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.
Type:
Grant
Filed:
April 9, 1998
Date of Patent:
July 4, 2000
Assignee:
Loma Linda University Medical
Inventors:
William J. Wechter, David E. Murray, Darko Kantoci, Barry H. Levine, Elaine J. Benaksas
Abstract: The present invention provides an composition for attracting noctuid and/or other lepidopteran species. Liquid and solid formulations are provided, along with methods for their use, for controlling or eliminating noctuid and/or other lepidopteran species, and/or protecting plants susceptible to noctuid and/or other lepidopteran species damage.
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
June 13, 2000
Assignee:
The United States of America as represented by the Secretary of Agriculture
Inventors:
Juan D. Lopez, Jr., Ted N. Shaver, Kenneth R. Beerwinkle, Peter D. Lingren
Abstract: The present invention is directed to the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions; compositions containing these compounds; and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 R.sub.11, n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, Y and Z are independently, 0, NH, or S.
Type:
Grant
Filed:
June 2, 1997
Date of Patent:
May 30, 2000
Assignee:
Avon Products, Inc.
Inventors:
Dmitri Ptchelintsev, Neil Scancarella, Robert Kalafsky
Abstract: The invention relates to a novel preserving system of at least one C.sub.1 -C4 alkyl para-hydroxybenzoate, sodium benzoate and N-(3-chloroallyl)hexaminium chloride. This combination finds its application most particularly in the cosmetic or pharmaceutical field, and in particular in cleansing compositions for the face and the eyes.
Abstract: Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.
Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.
Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
Abstract: Therapeutic treatment as well as prophylactic measures are provided by topical application of compositions containing an aryl 2-acetoxyethanoic acid to eradicate or prevent the development of axillary foul odor, foot malodor and other body odors, e.g. scalp, and skin, nail and follicular infections caused by microorganisms. The compositions are antimicrobial against several organisms that infect the skin and are specifically effective against P. acnes. The compositions are therapeutically effective against folliculitis and perifolliculitis and are useful for other skin lesions, nail and mucosal infections such as impetigo, seborrheic dermatitis, erythrasma and trichomycosis axillaris, associated with or caused by microorganisms. The therapeutic effect of the composition may be synergized or amplified by incorporating a cosmetic or dermatologic agent into the formulation for topical treatment of cosmetic and dermatologic indications.
Type:
Grant
Filed:
June 28, 1999
Date of Patent:
April 25, 2000
Assignee:
Tristrata, Inc. (A Delaware Corporation)
Abstract: Therapeutic treatment as well as prophylactic measures are provided by topical application of compositions containing an aryl 2-acetoxyethanoic acid to eradicate or prevent the development of axillary foul odor, foot malodor and other body odors, e.g. scalp, and skin, nail and follicular infections caused by microorganisms. The compositions are antimicrobial against several organisms that infect the skin and are specifically effective against P. acnes. The compositions are therapeutically effective against folliculitis and perifolliculitis and are useful for other skin lesions, nail and mucosal infections such as impetigo, seborrheic dermatitis, erythrasma and trichomycosis axillaris, associated with or caused by microorganisms. The therapeutic effect of the composition may be synergized or amplified by incorporating a cosmetic or dermatologic agent into the formulation for topical treatment of cosmetic and dermatologic indications.
Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.
Type:
Grant
Filed:
April 16, 1997
Date of Patent:
March 28, 2000
Assignee:
Novo Nordisk A/S
Inventors:
Henrik Sune Andersen, Niels Peter Hundahl M.o slashed.ller, Peter Madsen
Abstract: This invention relates to the use of benzonaphthalene compounds for the treatment of peripheral neuropathies, central neurodegenerative diseases and autoimmune diseases of the nervous system.
Type:
Grant
Filed:
January 8, 1999
Date of Patent:
March 28, 2000
Assignee:
Galderma Research & Development, S.N.C.
Inventors:
Xavier Vige, Jesus Benavides, Braham Shroot, Veronique Taupin
Abstract: Compositions are provided containing molecules having at least one moiety from .beta.-(3,4-dihydroxyphenyl) lactic acid and/or caffeic acid, which are found in extracts from the plant genus Salvia, said moieties being of the formula: ##STR1## the active agents having a molecular weight of at least 190 daltons. A class of preferred agents are those which are conjugated to form dimers, trimers, tetramers and larger polymers containing said moieties, with the most preferred being salvianolic acid dimers, trimers, tetramers and larger polymers. The compounds and compositions may be administered in pharmaceutically acceptable carriers and excipients systemically or locally to treat viral infections.
Type:
Grant
Filed:
June 25, 1999
Date of Patent:
March 28, 2000
Assignee:
Georgetown University School of Medicine
Abstract: The instant invention provides compositions containing molecules having at least one moiety from .beta.(3,4-dihydroxyphenyl) lactic acid and/or caffeic acid which are found in extracts from genus Salvia, said moieties being of the formula: ##STR1## said active agents having a molecular weight of at least 190 daltons. A class of preferred agents are those which are conjugated to form dimers and larger polymers containing said moieties. The agents of the invention may be administered in pharmaceutically acceptable carriers systemically or locally.
Type:
Grant
Filed:
June 25, 1998
Date of Patent:
March 14, 2000
Assignee:
Georgetown University School of Medicine
Abstract: This invention relates to a novel 2-hydroxypropionic acid derivative and its manufacturing method. Based on its mechanism to inhibit the CPT I, 2-hydroxypropionic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and fewer side effects.
Type:
Grant
Filed:
May 4, 1999
Date of Patent:
February 29, 2000
Assignees:
Sang Sup JEW, Kwang Ho KO, Bak Kwang KIM
Inventors:
Sang Sup Jew, Suk Ku Kang, Deuk Joon Kim, Won Ki Kim, Hwa Jung Kim, Chang Kiu Moon, Jeong Hill Park, Young Ger Suh, Bong Jin Lee, Jee Woo Lee, Ki Hwa Jung, Moon Woo Chun, Hoon Huh, Eung Seok Lee, Hyung Ook Kim, Eun Kyung Kim, Sung Jin Kim, Jae Hoon Cheong, Kwang Ho Ko, Bak Kwang Kim
Abstract: The present invention provides methods for treating cancer, particularly malignant tumors, with thyroxine analogues having no significant hormonal activity. A thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer. Particularly preferred thyroxine analogues are those capable of causing about 35 percent or more inhibition of initial velocity of microtubule protein assembly in vitro.
Abstract: A subject of the invention is the compounds of general formula (I): ##STR1## in which R1=H, alkyl, acyl, R2 and R3=H, alkyl, R4=aryl, heteroaryl, X=O, CH2, Y=OH, O-alkyl or NRaRb, as well as the salts, their preparation processes, the intermediates of these processes, their use as medicaments and the pharmaceutical compositions containing them.
Abstract: A non-toxic arthropod control composition is disclosed for application to foliage for plant protection. The composition includes behavior interfering compounds, agricultural oil and/or surface active compounds and diluents. The behavior interfering compounds may be any known conventional compound capable of interrupting or altering the normal behavioral sequences of the target. The agricultural oil can be a vegetable oil.
Abstract: Trienoic compounds having activity as antagonists for retinoic acid receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.
Abstract: Disclosed are nitrosated and nitrosylated .alpha.-adrenergic receptor antagonists, compositions of an .alpha.-adrenergic receptor antagonist (.alpha.-antagonist), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.cndot.); and uses for each of them in treating human impotence or erectile dysfunction.
Type:
Grant
Filed:
September 18, 1996
Date of Patent:
November 30, 1999
Assignee:
NitroMed, Inc.
Inventors:
David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
Abstract: This invention provides extracts of Salvia species essentially consisting of that fraction from a Salvia that precipitates from aqueous solution at pH .ltoreq.3, said precipitate having the property such that it is is essentially fully dissolved in aqueous solution at pH 6, with solubility beginning to be readily observable at about pH 4, said extract having a molecular weight of .ltoreq.3500 datons. A preferred embodiment of the invention provides active agents having a molecular weight of .ltoreq.1000 daltons.
Type:
Grant
Filed:
December 4, 1997
Date of Patent:
November 30, 1999
Assignee:
Georgetown University School of Medicine
Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.
Type:
Grant
Filed:
February 9, 1999
Date of Patent:
November 30, 1999
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Christopher I. Bayly, Cameron Black, Nathalie Ouimet, David Percival, Serge Leger, Marc Ouellet
Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
Type:
Grant
Filed:
December 18, 1997
Date of Patent:
November 30, 1999
Assignee:
Zambon Group S.p.A.
Inventors:
Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.
Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
Type:
Grant
Filed:
October 30, 1997
Date of Patent:
November 16, 1999
Assignee:
BASF Aktiengesellschaft
Inventors:
Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
Abstract: The present invention is drawn to the inhibition of activation of NF-.kappa.B by caffeic acid phenethyl ester (CAPE) and two analogues of CAPE. Tumor necrosis factor (TNF) activation of NF-.kappa.B is completely blocked by CAPE in a dose- and time-dependent manner, as is activation by phorbol ester, ceramide, hydrogen peroxide, and okadaic acid. Additionally, capsaicin (8-methyl-N-vanillyl-6-noneamide) and resiniferatoxin inhibit the activation of NF-.kappa.B induced by different agents.
Abstract: A method for treating skin conditions, such as rosacea and sensitive skin, that manifest as a tendency towards flushing and blushing is provided. Also provided herein, are compositions for the treatment of rosacea and sensitive skin that are comprised of at least one antioxidant selected from the following groups of antioxidants: (a) phenolic compounds that contain at least one hydroxyl group connected directly to a benzene ring and to another unsaturated chemical grouping, (b) sulfur-containing compounds that contain at least one sulfhydryl groups or sulfur-containing compounds that contain at least one disulfide group, or (c) polyene compounds that have conjugated systems of double bonds.
Abstract: Two new forms of prodrug for phenylacetate, of even congeners of phenylalkanoic acid and phenylalkenoic acids, which are the phenylalkanoic or phenylalkenoic esters of glycerol, or the ethyl esters of phenylalkanoic acid or phenylalkenoic acids. These forms of the drugs provide a convenient dosage form of the drugs. The prodrugs of the invention are useful to treat patients with diseases of nitrogen accumulation, patients with certain .beta.-hemoglobinopathies, anemia, and cancer.